Synthesis, biological evaluation and molecular modeling studies of arylidene-thiazolidinediones with potential hypoglycemic and hypolipidemic activities

Eur J Med Chem. 2007 Oct;42(10):1263-71. doi: 10.1016/j.ejmech.2007.02.015. Epub 2007 Mar 3.

Abstract

New arylidene-thiazolidinediones (ATZDs) were synthesized and evaluated in the alloxan-induced hyperglycemia mice model. The molecular target taken into consideration is the nuclear PPAR-gamma whose crystallographic structure is available on the PDB database as 2PRG. Thus the hypoglycemic and hypolipidemic activities of compounds were compared with the result of their docking after removal of the co-crystallized ligand present in the 2PRG structure. Molecular modeling studies were carried out using the Autodock 3.0.5 and ADT 1.1 programs.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alloxan / pharmacology
  • Animals
  • Blood Glucose / metabolism
  • Diabetes Mellitus, Experimental / chemically induced
  • Diabetes Mellitus, Experimental / drug therapy
  • Dose-Response Relationship, Drug
  • Hydrogen Bonding
  • Hypoglycemic Agents / chemical synthesis*
  • Hypoglycemic Agents / chemistry
  • Hypoglycemic Agents / therapeutic use*
  • Hypolipidemic Agents / chemical synthesis*
  • Hypolipidemic Agents / chemistry
  • Hypolipidemic Agents / therapeutic use*
  • Ligands
  • Mice
  • Models, Molecular
  • Molecular Structure
  • PPAR alpha / metabolism
  • PPAR gamma / metabolism
  • Thiazolidinediones / chemical synthesis*
  • Thiazolidinediones / chemistry
  • Thiazolidinediones / therapeutic use*
  • Triglycerides / blood

Substances

  • Blood Glucose
  • Hypoglycemic Agents
  • Hypolipidemic Agents
  • Ligands
  • PPAR alpha
  • PPAR gamma
  • Thiazolidinediones
  • Triglycerides
  • Alloxan